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RP-6306 + gemcitabine
- Development stage
- Phase 2
- Lead developer
- Repare Therapeutics
- Modality
- Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
- Administration
- Oral, Intravenous
01
Overview
RP-6306 + gemcitabine is a combination of an investigational small molecule inhibitor, RP-6306 (also known as Lunresertib), and the chemotherapeutic agent gemcitabine. RP-6306 specifically targets PKMYT1, a serine/threonine protein kinase involved in regulating the cell cycle, especially by inhibiting CDK1 phosphorylation. Inhibition of PKMYT1 by RP-6306 induces rapid mitotic entry, resulting in DNA damage and mitotic catastrophe, leading to PANoptosis—a cell death process relevant in cancer therapy. Gemcitabine, a nucleoside analog, inhibits DNA synthesis and is widely used in the treatment of various solid tumors. The combination of RP-6306 with gemcitabine is being studied for its potential synergistic anti-tumor activity, particularly enhancing tumor cell death and inhibiting tumor growth and metastasis in advanced solid tumors such as pancreatic ductal adenocarcinoma, bladder, breast, colon, kidney, liver, lung, melanoma, prostate, and stomach cancers. Current clinical trials are evaluating its safety, tolerability, pharmacokinetics, and preliminary efficacy[1][3][5][7][9].
- Other names
- RP-6306 + gemcitabine
02
Targets
PKMYT1 (Protein kinase membrane associated tyrosine/threonine 1)
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